AZOLE DERIVATIVES OF BENZENE Russian patent published in 2018 - IPC C07D417/10 A61K31/427 A61P3/06 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound represented by the formula (I), or a pharmaceutically acceptable salt thereof, wherein R₁ means OR, NRR', which can form a ring, or SR. Wherein R and R' independently mean hydrogen atom, linear, cyclic or branched alkyl containing 1-8 carbon atoms, and optionally substituted by one or more linear, circular, or branched alkoxygroup containing 1-8 carbon atoms, halogen atoms or hydroxyl groups, monocyclic or bicyclic aryl containing 6-10 carbon atoms, optionally substituted by one or more linear, cyclic or branched alkyl containing 1-8 carbon atoms, linear, cyclic or branched alkoxygroup containing 1-8 carbon atoms, or halogen atoms, where the term "NRR' forms a ring" means that R and R' join to form pyrrolidine-1-yl group; R₂ means a hydrogen atom or a linear, cyclic or branched alkyl containing 1-8 carbon atoms; X₁, X₂ and X₃ mean independently CR₃ or a nitrogen atom, or X₁ means CR₃ or a nitrogen atom, and X₂ and X₃ together form a benzene ring. Moreover, R₃ means a hydrogen atom or a linear, cyclic or branched alkyl having 1-8 carbon atoms. The invention also relates to specific compounds corresponding to formula (I). The invention relates to an intermediate compounds represented by the formulas, and , where R₁, R₂, X₁, X₂ and X₃ correspond to the values given for compounds of formula (I) and R₄ means protective group of the carboxylic group, selected from methyl, ethyl, isopropyl, heptyl, tert-butyl, methoxymethyl, methylthiomethyl, methoxyethoxymethyl, propanol and benzyl, and R₅ means a protective group of phenolic hydroxyl group selected from methyl, isopropyl, allyl, tert-butyl, methoxymethyl, methylthiomethyl, methoxyethoxymethyl, 1-ethoxyethyl, benzyl, 4-methoxybenzyl, acetyl, trimethylsilyl, t-butyldimethylsilyl. The compounds of the invention of formula (I) have an inhibitory activity against xanthine oxidase.

EFFECT: azole derivatives of benzene as inhibitors of xanthine oxidase.

19 cl, 15 tbl, 58 ex